mGluR3 Agonist

Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.

LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC₅₀ values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects.

Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC₅₀s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.

LY2934747 is a selective and blood-brain barrier-permeable dual mGlu2/mGlu3 receptor agonist, with K_i values of 260 nM and 177 nM, and EC₅₀ values of 8.4 nM and 62.4 nM against human receptors, respectively. LY2934747 exhibits antipsychotic and analgesic activities in in vivo animal models. LY2934747 can be used in studies related to psychosis and pain.

LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 K_i=0.927 nM，EC₅₀=0.47 nM; hmGlu2 K_i=412 nM，EC₅₀=47.5 nM).

LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with K_is of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.

DCG-IV is a potent agonist of group II mGluRs with EC₅₀s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC₅₀: mGlu1R/5R=389/630 μM) and III receptors (IC₅₀: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects.

Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.

Talaglumetad hydrochloride (LY-544344 hydrochloride) is an orally active prodrug of Eglumegad (HY-18941) and a metabotropic glutamate receptor 2/3 (mGluR2/3) agonist. Talaglumetad hydrochloride undergoes transmembrane transport via the intestinal peptide transporter hPepT1, and is enzymatically hydrolyzed to produce L-alanine and the parent drug Eglumegad after entering the body. Talaglumetad hydrochloride can be used in research related to metabotropic glutamate receptor 2-associated neurological systems.

LY2812223 is a highly potent, functionally selective mGlu₂ receptor agonist with mGlu₂ binding affinity for mGlu₂ and mGlu₃ (K_i=144 nM and 156 nM, respectively).

Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia.

MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.

MGS0028 is a selective metabotropic glutamate 2/3 (mGlu2/3) receptor agonist. MGS0028 can be used for psychiatric disorders research.

LBG30300 is a subtype-selective mGlu₂ receptor agonist EC₅₀ 0.6 nM. LBG30300 is blood-brain barrier permeable.

Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research.

MGS0008 is an orally active and brain-penetrant metabotropic glutamate receptor 2/3 (mGlu2/3) agonist with EC₅₀ values of 29.4 nM and 45.4 nM for mGluR2 and mGluR3, respectively. MGS0008 is promising for research of central nervous system disorders, including schizophrenia, anxiety, and neurodegenerative diseases.

LY459477 is a potent, selective and orally active metabotropic glutamate 2/3 receptor (mGluR2/3) agonist. LY459477 can effectively suppress Phencyclidine-evoked locomotor activity at doses that do not impair neuromuscular coordination. LY459477 can be used for the research of neurological disease.